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Assay Detail

CHEMBL3412296

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to human GST-thrombin-tagged MDM2 ( 1 to 188 aa) assessed as inhibition of interaction with human p53 preincubated with compound for 20 mins by HTRF assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

E3 ubiquitin-protein ligase Mdm2 (CHEMBL5023)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction.
Rew Y, Sun D, Yan X, Beck HP, Canon J, Chen A, Duquette J, Eksterowicz J, Fox BM, Fu J, Gonzalez AZ, Houze J, Huang X, Jiang M, Jin L, Li Y, Li Z, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, Oliner JD, Osgood T, Saiki AY, Shaffer P, Wang YC, Wortman S, Yakowec P, Ye Q, Yu D, Zhao X, Zhou J, Medina JC, Olson SH.
J Med Chem (2014) 57 : 10499 -10511
PubMed 25384157 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 9.45 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3407554 1 10.00
CHEMBL3125537 1 10.00
CHEMBL3407558 1 9.89
CHEMBL3236364 1 9.77
CHEMBL3407559 1 9.74
CHEMBL3407557 1 9.74
CHEMBL3407560 1 9.68
CHEMBL3407564 1 9.68
CHEMBL3407565 1 9.68
CHEMBL3407574 1 9.59
CHEMBL3407556 1 9.43
CHEMBL3407561 1 9.43
CHEMBL3407568 1 9.38
CHEMBL3407562 1 9.31
CHEMBL3407571 1 9.31
CHEMBL3407572 1 9.28
CHEMBL3125702 NAVTEMADLIN 3.0 1 9.20
CHEMBL3407567 1 9.14
CHEMBL3407570 1 9.10
CHEMBL3407573 1 9.08
CHEMBL3407566 1 8.74
CHEMBL3407563 1 8.62
CHEMBL3407555 1 -
CHEMBL3407569 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3407554 IC50 = 0.1 nM 10.00
CHEMBL3125537 IC50 = 0.1 nM 10.00
CHEMBL3407558 IC50 = 0.13 nM 9.89
CHEMBL3236364 IC50 = 0.17 nM 9.77
CHEMBL3407559 IC50 = 0.18 nM 9.74
CHEMBL3407557 IC50 = 0.18 nM 9.74
CHEMBL3407560 IC50 = 0.21 nM 9.68
CHEMBL3407564 IC50 = 0.21 nM 9.68
CHEMBL3407565 IC50 = 0.21 nM 9.68
CHEMBL3407574 IC50 = 0.26 nM 9.59
CHEMBL3407556 IC50 = 0.37 nM 9.43
CHEMBL3407561 IC50 = 0.37 nM 9.43
CHEMBL3407568 IC50 = 0.42 nM 9.38
CHEMBL3407562 IC50 = 0.49 nM 9.31
CHEMBL3407571 IC50 = 0.49 nM 9.31
CHEMBL3407572 IC50 = 0.52 nM 9.28
CHEMBL3125702 NAVTEMADLIN IC50 = 0.63 nM 9.20
CHEMBL3407567 IC50 = 0.73 nM 9.14
CHEMBL3407570 IC50 = 0.79 nM 9.10
CHEMBL3407573 IC50 = 0.83 nM 9.08
CHEMBL3407566 IC50 = 1.8 nM 8.74
CHEMBL3407563 IC50 = 2.4 nM 8.62
CHEMBL3407555 IC50 < 0.1 nM -
CHEMBL3407569 IC50 < 0.1 nM -